5-SUBSTITUTED AMINO-4-HYDROXY-PENTANOIC ACID DERIVATIVES AND THEIR USE

摘要

A 5-substituted amino-4-hydroxy-pentanoic acid derivative having the formula: wherein R<1> is a hydrogen atom, a lower alkoxycarbonyl group, an aryloxycarbonyl group, an aralkyloxycarbonyl group or a lower alkanoyl group which may be substituted by from one to three substituents selected from the group consisting of an amino group, a hydroxyl group, a carboxyl group, an aryloxy group, an aralkyloxycarbonylamino group, a lower alkoxycarbonylamino group wherein each of X<1> and X<2> which may be the same or different is a hydrogen atom, a lower alkyl group, an aryl group or an aralkyl group, or X<1> and X<2> form together with the adjacent nitrogen atom a 5- or 6-membered heterocyclic group which may further contain a hereto atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom which may further contain a double bond in its carbon chain, each of R<2>, R<3> and R<5> which may be the same or different is a hydrogen atom, a lower alkyl group or a residue of an acidic, neutral or basic amino acid, R<4> is a hydrogen atom or a lower alkyl group, R<6> is a lower alkyl, cycloalkyl, cycloalkylalkyl or aralkyl group which is substituted by one or two hydroxyl groups, R<7> is a hydroxyl group, a -OY group wherein Y is a lower alkyl group, an aryl group, an aralkyl group, a lower alkoxyalkyl group, a lower alkanoyloxyalkyl group, a lower alkoxycarbonyloxyalkyl group or a 1-phthalidyl group, wherein each of Y<1> and Y<2> which may be the same or different is a hydrogen atom, a lower alkyl group, an aryl group, an aralkyl group or a cycloalkyl group, or Y<1> and Y<2> form together with the adjacent nitrogen atom 5- or 5-membered heterocyclic group which may further contain a hereto atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, and each of n and m which may be the same or different is 0 or 1.